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CAS号 | 1803274-65-8 | 货号 | BCP18989 |
中文名 | BAY-1436032 | ||
英文名 | BAY-1436032 | ||
中文别名 | |||
英文别名 | BAY 1436032;BAY1436032; | ||
SMILES | |||
化学名称 | |||
分子式 | C26H30F3N3O3 | 分子量 | 489.53 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). BAY 1436032 is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displayed potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. In line with the proposed mode of action, a concentration-dependent lowering of 2-HG was observed in vitro accompanied by differentiation and maturation of mIDH1 tumor cells. Furthermore, BAY 1436032 showed a favourable selectivity profile against wtIDH1/2 and a large panel of off-targets in vitro. |
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